In vitro cytotoxic activity evaluation of phenytoin derivatives against human leukemia cells.

Hydantoin derivatives, including phenytoin (5,5-diphenylhydantoin), have recently gained attention as they possess a variety of important biochemical and pharmacological properties. Nevertheless, available information on anticancer activity of hydantoin derivatives is still scarce. Here, we evaluated possible antileukemic potential of four phenytoin analogs, namely: methyl 2-(2,4-dioxo-5,5-diphenylimidazolidin-3-yl)propanoate (1), methyl 2-(1-(3-bromopropyl)-2,4-dioxo-5,5-diphenylimidazolidin-3-yl)propanoate (2), 1-(3-bromopropyl)-3-methyl-5,5-diphenylimidazolidine-2,4-dione (3) and 1-(3-bromobutyl)-3-methyl-5,5-diphenylimidazolidine-2,4-dione (4). The experiments were performed on human acute histiocytic lymphoma U937 cells and human promyelocytic leukemia HL-60 cells. The present study was conducted using spectrophotometric 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide (MTT) assay and the electronic Beckman-Coulter method. We observed temporary changes in the leukemia cell viability, volume and count. The effects of the four 5,5-diphenylhydantoin derivatives on U937 and HL-60 cells depended on the agent tested and its concentration, the time intervals after the compound application, and the leukemia cell line used. HL-60 cells were more sensitive than U937 cells to the action of the phenytoin analogs (1-4). The antileukemic activities of the three bromoalkyl diphenylhydantoin derivatives (2, 3, and 4) were stronger than that of the compound 1 [methyl 2-(2,4-dioxo-5,5-diphenylimidazolidin-3-yl) propanoate], with no bromoalkyl substituent. The structural modifications of 5,5-diphenylhydantoin are responsible for such varied antileukemic potential of its four derivatives.

Isolamento, identificação e avaliação da atividade antileucêmica de alcaloides indólicos monoterpênicos de Tabernaemontana salzmannii (A. DC.), Apocynaceae / Isolation, identification and antileukemic activity of the monoterpene indole alkaloids from Tabernaemontana salzmannii (A. DC.), Apocynaceae

O presente trabalho descreve o isolamento e a identificação de nove alcaloides indólicos monoterpênicos das cascas das raízes e folhas de Tabernaemontana salzmannii (Apocynaceae). As estruturas dos alcaloides foram identificadas através de métodos espectroscópicos uni (RMN ¹H, 13C, APT) e bidimensionais (¹H-¹H-COSY, ¹H-¹H-NOESY, HMQC e HMBC) e espectrometria de massas (EM), além da comparação com dados de literatura. Um screening in vitro da atividade antileucêmica foi feito com os alcaloides majoritários isolados. Dentre os nove alcaloides isolados, a isovoacangina e voacangina mostraram-se capazes de induzir morte celular por apoptose em células leucêmicas humanas THP-1.

This work describes the isolation and structural determination of nine monoterpenic indole alkaloids from the roots bark and leaves of Tabernaemontana salzmannii. The alkaloids were identified by spectroscopic methods uni (NMR ¹H, 13C, APT) and two-dimensional (¹H-¹H-COSY, ¹H-¹H-NOESY, HMQC and HMBC) and mass spectra besides comparison with literature data. An in vitro screening was done with the isolated major alkaloids. Among the nine alkaloids isolated, isovoacangine and voacangine alkaloids were able to induce apoptosis cell death in human leukemic cells line THP-1.

Isolamento, identificação e avaliação da atividade antileucêmica de alcaloides indólicos monoterpênicos de Tabernaemontana salzmannii A. DC., Apocynaceae / Isolation, identification and antileukemic activity of the monoterpene indole alkaloids from Tabernaemontana salzmannii A. DC., Apocynaceae

O presente trabalho descreve o isolamento e a identificação de nove alcaloides indólicos monoterpênicos das cascas das raízes e folhas de Tabernaemontana salzmannii (Apocynaceae). As estruturas dos alcaloides foram identificadas através de métodos espectroscópicos uni (RMN ¹H, 13C, APT) e bidimensionais (¹H-¹H-COSY, ¹H-¹H-NOESY, HMQC e HMBC) e espectrometria de massas (EM), além da comparação com dados de literatura. Um screening in vitro da atividade antileucêmica foi feito com os alcaloides majoritários isolados. Dentre os nove alcaloides isolados, a isovoacangina e voacangina mostraram-se capazes de induzir morte celular por apoptose em células leucêmicas humanas THP-1.

This work describes the isolation and structural determination of nine monoterpenic indole alkaloids from the root barks and leaves of Tabernaemontana salzmannii. The alkaloids were identified by spectroscopic methods uni (NMR ¹H, 13C, APT) and two-dimensional (¹H-¹H-COSY, ¹H-¹H-NOESY, HMQC and HMBC) and mass spectra besides comparison with literature data. An in vitro screening was done with the isolated major alkaloids. Among the nine alkaloids isolated, isovoacangine and voacangine alkaloids were able to induce apoptosis cell death in human leukemic cells line THP-1.

Antileukemic activity of donor-derived NK cell in mice in vivo / 吉林大学学报(医学版)

0.05). The survival time of the second control group and experimental groups was much longer than that of the first control group (P